Sublingual aspirin tablet

ABSTRACT

Aspirin is the most commonly used antipyretic, analgesic, anti-inflammatory agent. The usual pain-relieving adult dosage is 300 to 600 mg. 
     To minimize frequent aspirin-induced gastric disturbance, many aspirin products contain buffering agents. Only a portion of the aspirin acts as aspirin, as part of the aspirin is decomposed into salicylic acid and acetic acid. Buffering agents cannot fully neutralize these acids along with the gastric acids, especially when larger aspirin doses are required. The likelihood of G I tolerance cannot be fully improved by any buffering agent. 
     Aspirin is effective within 15 to 25 minutes after swallowing.

The primary objects of my invention are: Faster action, no stomachirritation, convenient ingestion, full benefit of the aspirin bypreventing decomposition.

The objects of my invention have been achieved by making it possible toingest the aspirin sublingually by means of a tablet formulated to bepractically tasteless, which dissolves rapidly, uniformly, andcompletely under the tongue. It is absorbed without being decomposed, itis not irritation, it goes immediately into the blood stream, and itproduces no stomach disturbance. Furthermore it's action is super-fast:it is effective within 3 to 5 minutes.

The harmless, edible inert ingredients added to the aspirin in verysmall amounts and proper proportions stabilize the aspirin, neutralizethe taste, minimize any possible irritation, and make the tablet porousto effect fast solubility and absorbtion by the blood vessels under thetongue without decomposition of the aspirin.

DESCRIPTION OF THE INVENTION

This invention is concerned with a novel, practical method of ingestingan aspirin tablet; such a tablet is to be placed under the tongue.

The purpose of this method is: faster action, faster relief of pain,elimination of the necessity to use water or other liquid forswallowing, and avoidance of gastric disturbance; the prevention ofaspirin decomposition into Acetic Acid and Salicylic Acid in thestomach. The sublingual tablet enters the bloodstream directly.

Obviously, such a tablet, when placed under the tongue, must dissolvecompletely and rapidly without objectionable taste or irritation. Theseand other objects of the present invention have been accomplished byadding to the Aspirin several components which neutralize the Aspirintaste, effect the absorbtion by the blood vessels under the tongue, andgive the compressed tablet a certain porosity. None of the ingredientsused chemically decomposes the Aspirin.

This has all been achieved in such a way that the complete mixture ofAspirin plus the other components is directly compressible by means ofthe conventional manufacturing procedures.

The single components of my invention are: Granulated Sugar, Mannitol,Sodium Citrate anhydrous, Calcium Glycero Phosphate, Mineral Oil, anon-ionic hydrophilic surfactant, a non-ionic lipophilic surfactant, andGlycerine.

Granulated Sugar is the excipient; Mannitol, Sodium Citrate anhydrous,and Calcium Glycero Phosphate are the taste neutralizers. Mineral Oil,Glycerine, and the two surfactants are the components which effect thevitally essential rapid dissolving of the tablet under the tongue bymaking the tablet porous; whereby even the smallest amount of salivaforms an emulsion effecting fast and uniform tablet dissolution andimproving the desired absorbability of the tablet.

All the ingredients are compatible with one another. The very easilydecomposable Aspirin remains undecomposed. Sodium Citrate anhydrousenhances the absorbability of Aspirin. The Mannitol in conjunction withthe smallest amount of a Calcium compound, i.e. Calcium GlyceroPhosphate, is the primary taste neutralizer.

Sugar, being a stabilizer of Aspirin, enters the blood stream togetherwith all the other components, thereby enhancing uniform absorbtionunder the tongue.

The amounts and the proportions of each of the components of myinvention are critical in the achievement of the objects of thisinvention. The optimum amounts of each component of my invention are:

    ______________________________________                                        Aspirin               100 parts                                               Granulated Sugar      150 to 180 parts                                        Mannitol              10 to 18 parts                                          Sodium Citrate anhydrous                                                                            3 to 4 parts                                            Calcium Glycero Phosphate                                                                           1 to 2 parts                                            Mineral Oil           3 to 5 parts                                            Glycerine             1 to 1.5 parts                                          Non-ionic lipophilic                                                          surfactant            .3 to .4 parts                                          Non-ionic hydrophilic                                                         ______________________________________                                    

The characteristics of the present invention will be further understoodby reference to the following examples.

EXAMPLES

The following examples illustrate the invention, but do not limit theinvention.

EXAMPLE 1

    ______________________________________                                        Part A:  Blend uniformly together -                                                    Aspirin (40 mesh)     300 g                                                   Mannitol              20 g                                                    Sodium Citrate anhydrous                                                                            10 g                                                    Calcium Glycero Phosphate                                                                           3 g                                            Part B:  Blend uniformly together -                                                    Granulated Sugar      550 g                                                   Mineral Oil           12 g                                                    Glycerine             3 g                                                     Non-ionic hydrophilic surfactant                                                                    1 g                                                     Non-ionic lipophilic surfactant                                                                     1 g                                                                           900 g                                          ______________________________________                                         Blend Part A with Part B and compress directly with medium pressure to        make 1000 tablets, each weighing 0.9 g and each containing 0.3 g Aspirin.

EXAMPLE 2

    ______________________________________                                        Part A:  Blend together -                                                              Aspirin (40 mesh)     330 g                                                   Granulated Sugar      530 g                                                   Mannitol              25 g                                                    Sodium Citrate anhydrous                                                                            12 g                                                    Calcium Glycero Phosphate                                                                           3 g                                            Part B:  Make a mixture of -                                                           Mineral Oil           15 g                                                    Glycerine             4 g                                                     Non-ionic hydrophilic surfactant                                                                    1 g                                                     Non-ionic lipophilic surfactant                                                                     921 g                                          ______________________________________                                         Blend Part B with Part A and press directly with medium pressure to make      1000 tablets, each weighing 0.921 g and each containing 0.33 g Aspirin.       Preferred Nonionic hydrophilic surfactant: Polysorbate 80.                    Preferred Nonionic lipophilic surfactant: Atmos 300                      

I claim:
 1. A sublingual rapidly soluble practically tasteless,non-irritating and stable aspirin tablet comprising:

    ______________________________________                                        Aspirin             100 parts                                                 Granulated Sugar    150 to 180 parts                                          Mannitol            10 to 18 parts                                            Sodium Citrate Anhydrous                                                                          3 to 4 parts                                              Calcium Glycerophosphate                                                                          1 to 2 parts                                              Mineral Oil         3 to 5 parts                                              Glycerine           1 to 1.5 parts                                            Non-ionic lipophilic                                                           surfactant         .3 to .4 parts                                            Non-ionic hydrophilic                                                          surfactant         .3 to .4 parts                                            ______________________________________                                    

wherein all parts are by weight, said non-ionic hydrophilic surfactanthaving an HLB of from 15 to 17 and said non-ionic lipophilic surfactanthaving an HLB of from 2 to 5.